Publications of Prof. Dr. Andreas Link


Piotr H. Małecki, Georg M. Fassauer, Nicole Rüger, Lukas Schulig, Andreas Link, Oxana Krylova, Udo Heinemann, Manfred S. Weiss: Structure-Based Mapping of the Histone-Binding Pocket of KDM4D Using Functionalized Tetrazole and Pyridine Core Compounds, Eur. J. Med. Chem. 2024, In Press, Journal Pre-proof, Available online 2 July 2024.

Felix Potlitz, Gottfried J. Palm, Anja Bodtke, Michael Lammers, Dennis Schade and Andreas Link: A Novel C3/C4-Fused Indole Scaffold through Acid-Catalyzed Cascade Reaction, Molecules 2024, 29, 13, 3064.

Daniel Längle, Stephanie Wojtowicz-Piotrowski, Till Priegann, Niklas Keller, Fabian Wesseler, Elena S. Reckzeh, Karsten Steffens, Christoph Grathwol, Jana Lemke, Maren Flasshoff, Christian Näther, Anna C. Jonson, Andreas Link, Oliver Koch, Gianni M. Di Guglielmo, and Dennis Schade: Expanding the Chemical Space of Transforming Growth Factor-β (TGFβ) Receptor Type II Degraders with 3,4-Disubstituted Indole Derivatives, ACS Pharmacol. Transl. Sci. 2024, 7, 4, 1069–1085.


Kristin Beirow, Julia Jedamzik, Lukas Schulig, Konrad W. Wurm, Christian J. Lemmerhirt, Robert K. Hofstetter, Andreas Link, Patrick J. Bednarski: Structure-Activity Relationships of Flupirtine Analogues for Liver Esterase-Mediated Cleavage of the 4-Fluorobenzylamine Moiety and Its Possible Relevance to Liver Toxicity, ChemMedChem 2023, 18, e202300145.

David Mainka, Julius Krause, Linus Großmann, Andreas Link, Lukas Schulig: Affordable and Easy Data Exploration of NIR Spectra Using Chemometric Techniques. J. Chem. Educ. 2023, 100, 2435–2441.

Mohsen Ahmadi, Debora Singer, Felix Potlitz, Zahra Nasri, Thomas von Woedtke, Andreas Link, Sander Bekeschus, Kristian Wende: Cold Physical Plasma-Mediated Fenretinide Prodrug Activation Confers Additive Cytotoxicity in Epithelial Cells, Antioxidants 2023, 12, 1271.

Felix Potlitz, Andreas Link, Lukas Schulig: Advances in the discovery of new chemotypes through ultra-large library docking, Exp. Opin. Drug Discov. 2023, 18, 3, 303–313.

Frieda-Marie Bartz, Kristin Beirow, Konrad Wurm, Daniel Baecker, Andreas Link, Patrick J. Bednarski: A graphite furnace-atomic absorption spectrometry-based rubidium efflux assay for screening activators of the Kv7.2/3 channel, Arch. Pharm. 2023, 356, 5, e2200585.

Konrad W. Wurm, Frieda-Marie Bartz, Lukas Schulig, Anja Bodtke, Patrick J. Bednarski, Andreas Link: Replacing the oxidation-sensitive triaminoaryl chemotype of problematic KV7 channel openers: Exploration of a nicotinamide scaffold, Arch. Pharm. 2023, 356, 2, e2200473.


Konrad W. Wurm, Frieda-Marie Bartz, Lukas Schulig, Anja Bodtke, Patrick J. Bednarski, Andreas Link: Carba Analogues of Flupirtine and Retigabine with Improved Oxidation Resistance and Reduced Risk of Quinoid Metabolite Formation, ChemMedChem 2022, 17, 16, e202200262.

Lukas Schulig, Norman Geist, Mihaela Delcea, Andreas Link, Martin Kulke: Fundamental Redesign of the TIGER2hs Kernel to Address Severe Parameter Sensitivity, J. Chem. Inf. Model 2022, 62, 17, 4200–4209.

Mohsen Ahmadi, Felix Potlitz, Andreas Link, Thomas von Woedtke, Zahra Nasri, Kristian Wende: Flucytosine-based prodrug activation by cold physical plasma, Arch. Pharm. 2022, 355, e2200061.

Konrad W. Wurm, Frieda-Marie Bartz, Lukas Schulig, Anja Bodtke, Patrick J. Bednarski, Andreas Link: Modifications of the triaminoaryl metabophore of flupirtine and retigabine aimed at avoiding quinone diimine formation, ACS Omega 2022, 7, 7989–8012.

Steven Behnisch-Cornwell, Christoph W. Grathwol, Lukas Schulig, Anika Voigt, Daniel Baecker, Andreas Link and Patrick J. Bednarski: Correlation Analysis of Protein Expression of 10 HDAC/Sirtuin Isoenzymes with Sensitivities of 23 Anticancer Drugs in 17 Cancer Cell Lines and Potentiation of Drug Activity by Co-Treatment with HDAC Inhibitors, Cancers 2022, 14, 187.


Piotr Grabarczyk, Martin Delin, Dorota Rogińska, Lukas Schulig, Hannes Forkel, Maren Depke, Andreas Link, Bogusław Machaliński, Christian A. Schmidt: Nuclear import of BCL11B is mediated by a classical nuclear localization signal and not the Krüppel-like zinc fingers, J. Cell Sci. 2021, 134, jcs258655.

Robert K. Hofstetter, Lukas Schulig, Jonas Bethmann, Michael Grimm, Maximilian Sager, Philipp Aude, Rebecca Kessler, Simon Kim, Werner Weitschies, Andreas Link: Supercritical fluid extraction-supercritical fluid chromatography of saliva: Single-quadrupole mass spectrometry monitoring of caffeine for gastric emptying studies, J. Sep. Sci. 2021, 44, 3700-3716.

Mahmoud Hasan, Christiane Modess, Tarek Roustom, Anne Dokter, Markus Grube, Andreas Link, Hélène Rey, Stefanie Adler, Konrad Meissner, Werner Siegmund: Chiral Pharmacokinetics and Metabolite Profile of Prolonged-release Ketamine Tablets in Healthy Human Subjects, Anesthesiology 2021, 135, 326-339.

Martin Kulke, Felix Nagel, Lukas Schulig, Norman Geist, Marcel Gabor, Julia Mayerle, Markus M Lerch, Andreas Link, Mihaela Delcea: A Hypothesized Mechanism for Chronic Pancreatitis Caused by the N34S Mutation of Serine Protease Inhibitor Kazal-Type 1 Based on Conformational Studies, J. Inflamm. Res. 2021, 14, 2111–2119.

Lukas Schulig, Piotr Grabarczyk, Norman Geist, Martin Delin, Hannes Forkel, Martin Kulke, Mihaela Delcea, Christian A. Schmidt, Andreas Link: Unveiling the N-Terminal Homodimerization of BCL11B by Hybrid Solvent Replica-Exchange Simulations, Int. J. Mol. Sci. 2021, 22, 3650.

Qingyun Tang, Christoph W. Grathwol, Aşkın S. Aslan-Üzel, Shuke Wu, Andreas Link, Christoffel Badenhorst, Ioannis Pavlidis, Uwe Bornscheuer: Directed evolution of a halide methyltransferase enables biocatalytic synthesis of diverse SAM analogues, Angew. Chem. Int. Ed. 2021, 60, 1524–1527,, Angew. Chem. 2021, 133, 1547–1551.

Sascha Grobe, Christoffel Badenhorst, Thomas Bayer, Emil Hamnevik, Shuke Wu, Christoph W. Grathwol, Andreas Link, Sven Koban, Henrike Brundiek, Beatrice Großjohann, Uwe Bornscheuer: Engineering Regioselectivity of a P450 Monooxygenase Enables the Synthesis of Ursodeoxycholic Acid via 7-beta-Hydroxylation of Lithocholic Acid, Angew. Chem. Int. Ed. 2020, 60, 753–757,, Angew. Chem. 2021, 133, 764–768.


Christoph W. Grathwol, Nathalie Wössner, Steven Behnisch-Cornwell, Lukas Schulig, Lin Zhang, Oliver Einsle, Manfred Jung and  Andreas Link: Activation of sirtuin 2 inhibitors employing photoswitchable geometry and aqueous solubility, ChemMedChem 2020, 15, 1480-1489.

Qingyun Tang, Yoanes Maria Vianney, Klaus Weisz, Christoph W. Grathwol, Andreas Link, Uwe T. Bornscheuer, Ioannis V. Pavlidis, Influence of substrate binding residues on the substrate scope and regioselectivity of a plant O-methyltransferase against flavonoids, ChemCatChem, 2020, 12, 3721-3727.


Christoph W. Grathwol, Nicolas Chrysochos, Benedict Elvers, Andreas Link, Carola Schulzke: Crystal structure of benzo[h]quinoline-3-carboxamide. Acta Cryst. 2019, E75, 1828-1832.

David Mainka, Andreas Link: Near-infrared spectroscopic identification and quantification of active pharmaceutical ingredients in closed capsules: a feasibility study for pediatric doses, Anal. Methods 2019, 11, 5185-5194.  

Christoph W. Grathwol, Nathalie Wössner, Sören Swyter, Adam C. Smith, Enrico Tapavicza, Robert K. Hofstetter, Anja Bodtke, Manfred Jung, Andreas Link: Azologization and repurposing of a hetero-stilbene based kinase inhibitor: Towards the design of photoswitchable sirtuin inhibitors, Beilstein J. Org. Chem. 2019, 15, 2170-2183.

Piotr H. Malecki, Nicole Rüger, Martin Roatsch, Oxana Krylova, Andreas Link, Manfred Jung, Udo Heinemann, Manfred S. Weiss: Structure-based screening of tetrazolylhydrazide inhibitors vs. KDM4 histone demethylases, ChemMedChem 2019, 14, 1828-1839.

Norman Geist, Martin Kulke, Lukas Schulig, Andreas Link, Walter Langel: Replica-Based Protein Structure Sampling Methods II: Advanced Hybrid Solvent TIGER2hs, J. Phys. Chem. B 2019, 123, 5995-6006.

Robert K. Hofstetter, Mahmoud Hasan, Carolin Eckert, Andreas Link: Supercritical fluid chromatography (Subtitle: From science fiction to scientific fact), ChemTexts 2019, 5,

Robert K. Hofstetter, Felix Potlitz, Lukas Schulig, Simon Kim, Mahmoud Hasan, Andreas Link: Subcritical Fluid Chromatography at Sub-Ambient Temperatures for the Chiral Resolution of Ketamine Metabolites with Rapid-Onset Antidepressant Effects, Molecules 2019, 24, 1927;

Robert K. Hofstetter, Benedict J. Elvers, Felix Potlitz, Andreas Link, Carola Schulzke: Crystal structure of 7,8,15,16,17-pentathiadispiro[]heptadecane. Acta Cryst. 2019, E75, 888-891.

Robert K. Hofstetter, Mahmoud Hasan, Georg M. Fassauer, Christian Bock, Abdrrahman S. Surur, Steven Behnisch, Christoph W. Grathwol, Felix Potlitz, Tobias Oergel, Werner Siegmund, Andreas Link: Simultaneous quantification of acidic and basic flupirtine metabolites by supercritical fluid chromatography according to European Medicines Agency validation, J. Chromatogr. A 2019, 1603, 338-347.

Christian Bock, Abdrrahman S. Surur, Kristin Beirow, Markus K. Kindermann, Lukas Schulig, Anja Bodtke, Patrick J. Bednarski, and Andreas Link: Sulfide Analogues of Flupirtine and Retigabine with Nanomolar KV7.2/KV7.3 Channel Opening Activity, ChemMedChem 2019, 14, 952-964. 

Abdrrahman S. Surur, Christian Bock, Kristin Beirow, Konrad Wurm, Lukas Schulig, Werner Siegmund, Patrick J. Bednarski and Andreas Link: Flupirtine and retigabine as templates for ligand-based drug design of KV7.2/3 activators, Org. Biomol. Chem. 2019, 17, 4512-4522.

Steffen Vojacek, Lukas Schulig, Nathalie Wössner, Norman Geist, Walter Langel, Manfred Jung, Dennis Schade, and Andreas Link: Tetrahydroindoles as Multipurpose Screening Compounds and Novel Sirtuin Inhibitors, ChemMedChem 2019, 14, 853-864.

Abdrrahman S. Surur, Kristin Beirow, Christian Bock, Lukas Schulig, Markus K. Kindermann, Anja Bodtke, Werner Siegmund, Patrick J. Bednarski, Andreas Link: Flupirtine Analogues: Explorative Synthesis and Influence of Chemical Structure on KV7.2/KV7.3 Channel Opening Activity, ChemistryOpen 2019, 8, 41-44.  

Christian Bock, Andreas Link: How to Replace the Lost Keys? Strategies Towards Safer KV7 Channel Openers, Future Med. Chem. 2019, 11, 337–355.

Abdrrahman S. Surur, Lukas Schulig, and Andreas Link: Interconnection of sulfides and sulfoxides in medicinal chemistry, Arch. Pharm. Chem. Life Sci. 2019, 352: e1800248. 



Christian Bock, Kristin Beirow, Abdrrahman S. Surur, Lukas Schulig, Anja Bodtke, Patrick J. Bednarski and Andreas Link: Synthesis and potassium KV7 channel opening activity of thioether analogues of the analgesic flupirtine, Org. Biomol. Chem. 2018, 16, 8695-8699.

Robert Hofstetter, Georg M. Fassauer, Andreas Link: The many (inter-)faces of supercritical fluid chromatography: the present and future prospects of online supercritical fluid extraction–supercritical fluid chromatography, Bioanalysis 2018, 10, 1073-1076.

Robert Hofstetter, Georg M. Fassauer, Andreas Link: Supercritical fluid extraction (SFE) of ketamine metabolites from dried urine and on-line quantification by supercritical fluid chromatography and single mass detection (on-line SFE–SFC–MS), J. Chromatogr. B 2018, 1076, 77-83.



Georg M. Fassauer, Robert Hofstetter, Mahmoud Hasan, Stefan Oswald, Christiane Modeß, Werner Siegmund, Andreas Link: Ketamine metabolites with antidepressant effects: Fast, economical, and eco-friendly enantioselective separation based on supercritical-fluid chromatography (SFC) and single quadrupole MS detection, J. Pharm. Biomed. Anal. 2017, 139, 410-419.

Steffen Vojacek, Katja Beese, Zayan Alhalabi, Sören Swyter, Anja Bodtke, Carola Schulzke, Manfred Jung, Wolfgang Sippl, and Andreas Link: Three-Component Aminoalkylations Yielding Dihydronaphthoxazine-Based Sirtuin Inhibitors: Scaffold Modification and Exploration of Space for Polar Side-Chains, Arch. Pharm. Chem. Life Sci., 2017, 350, n/a, e1700097. doi:10.1002/ardp.201700097.

Ulrike Schulz, Antje Grossmann, Felix Wilde, Marcus Freitag, Christian Lemmerhirt, Carola Schulzke, Andreas Link, Olaf Morgenstern: Synthesis, chemical behaviour, structure elucidation and iNOS inhibitory activity of 1-substituted 3-methylsulfanyl-5,6,7,8-tetrahydro-1H-[1,2,4]-triazolo[1,2-a]pyridazines; Pharmazie, 2017, 72, 371-382. 

Mahmoud Hasan, Robert Hofstetter, Georg M. Fassauer, Andreas Link, Werner Siegmund, Stefan Oswald: Quantitative chiral and achiral determination of ketamine and its metabolites by LC-MS/MS in human serum, urine and fecal samples, J. Pharm. Biomed. Anal. 2017, 139, 87-97.

Nicole Rüger, Georg M. Fassauer, Christian Bock, Thomas Emmrich, Anja Bodtke, and Andreas Link: Substituted tetrazoles as multipurpose screening compounds, Mol. Divers. 2017, 21, 9-27. 



Andreas Link and Christa E. Müller: G potein-coupled receptors: sustained signalling via intracellular megaplexes and pathway specific drugs, Angew. Chem. Int. Ed. 2016, 55, 15962-15964.

Andreas Link und Christa E. Müller: G-Protein-gekoppelte Rezeptoren: intrazelluläre Megaplexe und funktionell selektive Wirkstoffe, Angew. Chem. 2016, 128, 16194-16196.

Andreas Link und Hermann Wätzig: Gute NIR-Praxis: Moderne Infrarotspektrometrie in der Apotheke, Wissenschaftliche Verlagsgesellschaft, Stuttgart; 2016, ISBN-10: 3804734561, ISBN-13: 978-3804734562.



Nicole Rüger, Martin Roatsch, Thomas Emmrich, Henriette Franz, Roland Schüle, Manfred Jung, and Andreas Link: Tetrazolylhydrazides as Selective Fragment-Like Inhibitors of the JumonjiC-Domain-Containing Histone Demethylase KDM4A. ChemMedChem, 2015, 10, 1875-1883.

Christian J. Lemmerhirt, Mirko Rombach, Anja Bodtke, Patrick J. Bednarski, and Andreas Link: Oxidation Potentials of N-Modified Derivatives of the Analgesic Flupirtine Linked to Potassium KV7 Channel Opening Activity But Not Hepatocyte Toxicity. ChemMedChem, 2015, 10, 368-379.



Felix Wilde, Edgar Specker, Martin Neuenschwander, Marc Nazaré, Anja Bodtke, and Andreas Link: Tractable synthesis of multipurpose screening compounds with underrepresented molecular features for an open access screening platform. Mol. Divers., 2014, 18, 483-495.

Felix Wilde, Heidi Lemmerhirt, Thomas Emmrich, Patrick J. Bednarski, and Andreas Link: Microwave-assisted synthesis and evaluation of acylhydrazones as potential inhibitors of bovine glutathione peroxidase. Mol. Divers., 2014, 18, 307-322.

Vida Zohrabi-Kalantari, Felix Wilde, Renate Grünert, Patrick J. Bednarski, and Andreas Link: 4-Aminocyclopentane-1,3-diols as Platforms for Diversity: Synthesis of a Screening Library. Med. Chem. Comm., 2014, 5, 203-213.

Felix Wilde, Chamseddin Chamseddin, Heidi Lemmerhirt, Patrick J. Bednarski, Thomas Jira, and Andreas Link: Evaluation of (S)- and (R)-Misonidazole as GPX Inhibitors: Synthesis, Characterization Including Circular Dichroism and In Vitro Testing on Bovine GPx-1. Arch. Pharm. Chem. Life Sci., 2014, 347, 153-160.



Felix Wilde and Andreas Link: Advances in the design of a multipurpose fragment screening library. Expert Opin. Drug. Discov., 2013, 8, 597-606.

Vida Zohrabi-Kalantari, Abbas Jarrahian, Caterina Bissantz, Donald E. Bergstrom, Eric L. Barker, and Andreas Link: 4-Aminocyclopentane-1,3-diols as Platforms for Diversity: Synthesis of Anandamide Analogs. Med. Chem., 2013, 9, 881-888.



Riad Schulz, Thomas Emmrich, Heidi Lemmerhirt, Ulrike Leffler, Kristin Sydow, Carsten Hirt, Thomas Kiefer, Andreas Link, and Patrick J. Bednarski: Identification of a glutathione peroxidase inhibitor that reverses resistance to anticancer drugs in human B-cell lymphoma cell lines. Bioorg. Med. Chem. Lett., 2012, 22, 6712-6715.

Rogério Gaspar, Buket Aksu, Alain Cuine, Meindert Danhof, Milena Jadrijevic-Mladar Takac, Hans H. Lindén, Andreas Link, Eva-Maria Muchitsch, Clive G. Wilson, Per Öhrngren, and Lennart Dencker: Towards a European Strategy for Medicines Research (2014-2020): The EUFEPS Position Paper on Horizon 2020. Eur. J. Pharm. Sci., 2012, 47, 979-987.

Yousheng Guan, Caterina Bissantz, Donald E. Bergstrom, and Andreas Link: 1,2,4-Trisubstituted Cyclopentanes as Platforms for Diversity. Arch. Pharm. Chem. Life Sci., 2012, 345, 677-686.

Christoph Kamper, Katharina Korpis, Edgar Specker, Lennart Anger, Martin Neuenschwander, Patrick J. Bednarski, and Andreas Link: Sustainable synthesis and automated deposition: an accessible discovery screening library of fragment-like purines. Mol. Divers., 2012, 16, 541-551.



Marcus Freitag, Jörg Schemies, Tim Larsen, Khattab El Gaghlab, Felix Schulz, Tobias Rumpf, Manfred Jung, and Andreas Link: Synthesis and biological activity of splitomicin analogs targeted at human NAD+-dependent histone deacetylases (sirtuins). Bioorg. Med. Chem., 2011, 19, 3669-3677.

Ulrike Nagel, Gregor Radau, and Andreas Link: Short synthesis of ethyl 3-(3-aminophenyl)propanoate. Arch. Pharm. Chem. Life Sci., 2011, 344, 840-842.




Thomas Emmrich, Ali El-Tayeb, Hesham Taha, Roland Seifert, Christa E. Müller, and Andreas Link: Synthesis of a hydrolytically stable fluorescent-labeled ATP analog as a tool for probing adenylyl cyclases. Bioorg. Med. Chem. Lett., 2010, 20, 232-235.

Vida Zohrabi-Kalantari, Philipp Heidler, Marcel Kaiser, Reto Brun, Christoph Kamper, and Andreas Link: Inhibitors of Adenosine Consuming Parasites Through Polymer-Assisted N-Acylation of N6-substituted 5'-Amino-5'-deoxyadenosines. Mol. Divers., 2010, 14, 307-320.

Andreas Link, Philipp Heidler, Marcel Kaiser, Reto Brun: Parallel synthesis of a series of non-functional ATP/NAD-analogues with activity against trypanosomatid parasites. Mol. Divers., 2010, 14, 215-224.



Andreas Link, Philipp Heidler, Marcel Kaiser, Reto Brun: Synthesis of a series of N6-substituted adenosines with activity against trypanosomatid parasites. Eur. J. Med. Chem., 2009, 44, 3665-3671.

Philipp Heidler, Vida Zohrabi-Kalantari, Marcel Kaiser, Reto Brun, Thomas Emmrich, and Andreas Link: Inhibitors of adenosine consuming prasites through polymer-assisted solution phase synthesis of lipophilic 5'-amido-5'-deoxyadenosine derivatives. Bioorg. Med. Chem., 2009, 17, 1428-1436.



Timothy Haemers, Jochen, Wiesner, Dirk Gießmann, Thomas Verbrugghen, Ulrik Hillaert, Regina Ortmann, Hassan Jomaa, Andreas Link, Martin Schlitzer, and Serge Van Calenbergh: Synthesis of β- and γ-oxa isosteres of fosmidomycin and FR900098 as antimalarial candidates, Bioorg. Med. Chem., 2008, 16, 3361-3371.

Dirk Gießmann, Philipp Heidler, Timothy Haemers, Serge Van Calenbergh, Armin Reichenberg, Hassan Jomaa, Claus Weidemeyer, Silke Sanderbrand, Jochen Wiesner, and Andreas Link: Towards new antimalarial drugs: Synthesis of non-hydrolyzable phosphate mimics as feed for a predictive QSAR study on 1-deoxy-D-xylulose-5-phosphate reductoisomerase inhibitors, Chem. Biodiv., 2008, 5, 643-656.



Andreas Link and Holger Stark: Designs that Enrich Lives, Arch. Pharm. Chem. Life Sci., 2007, 340, 509-510.

Marcus Freitag, Marcel Kaiser, Tim Larsen, Vida Zohrabi-Kalantari, Philipp Heidler, and Andreas Link: Synthesis and antiplasmodial activity of new N-[3-(4-piperazin-1-yl)propyl]carboxamides, Bioorg. Med. Chem., 2007, 15, 2782-2788.



Andreas Link und Gregor Radau: Phenol-Nachweis mittels 4-Aminophenazon nach Emerson. Pharmazie, 2006, 61, 801-802.

Conrad Kunick, Carola Bleeker, Christian Prühs, Frank Totzke, Christoph Schächtele, Michael H.G. Kubbutat, and Andreas Link: Matrix compare analysis discriminates subtle structural differences in a family of novel antiproliferative agents, diaryl-3-hydroxy-2,3,3a,10a-tetrahydrobenzo[b]cyclopenta[e]azepine-4,10(1H,5H)-diones. Bioorg. Med. Chem. Lett., 2006, 16, 2148-2153.



Vida Zohrabi-Kalantari, Philipp Heidler, Tim Larsen, and Andreas Link: O,N,N'-Trialkylisoureas as Mild Activating Reagents for N-Acylsulfonamide Anchors. Org. Lett. 7, 2005, 25, 5665-5667.

Tim Larsen und Andreas Link: Bioverfügbarkeit oral applizierter Wirkstoffe: zeitabhängig revidiert. Angew. Chem., 2005, 117, 4506-4208.

Tim Larsen and Andreas Link: A timely reassessment of early prediction in the bioavailability of orally administered drugs. Angew. Chem. Int. Ed., 2005, 44, 4432-4434.

Philipp Heidler and Andreas Link: Naked-Eye Bead Property Estimation Using a Red Safety-Catch Linker. Aust. J. Chem., 2005, 58, 182-187.

Philipp Heidler and Andreas Link: 4-(4-Sulfamoylphenylazo)benzoic acid as a red safety-catch linker. J. Sulf. Chem., 2005, 26, 3-6.

Philipp Heidler, Vida Zohrabi-Kalantari, Thierry Camels, Marc Capet, Isabelle Berrebi-Bertrand, Jean-Charles Schwartz, Holger Stark, and Andreas Link: Parallel synthesis and dopamine D3/D2 receptor screening of novel carboxamides. Bioorg. Med. Chem., 2005, 13, 2009-2014.

Philipp Heidler and Andreas Link: N-Acyl-N-alkyl-sulfonamide anchors derived from Kenner's safety-catch linker: powerful tools in bioorganic and medicinal chemistry. Bioorg. Med. Chem., 2005, 13, 575-599 (s. Titelbild des Hefts Nr. 3).



Vida Zohrabi-Kalantari and Andreas Link: Practical Synthesis of Fenbufen Ethanolamide. Arch. Pharm. Pharm. Med. Chem., 2004, 337, 546-548.

Claudia Herforth, Philipp Heidler, Stephan Franke, and Andreas Link: Polymer-bound reagents for the introduction of spacer-modified biotin labels. Bioorg. Med. Chem., 2004, 12, 2895-2902.

Claudia Herforth, Jochen Wiesner, Philipp Heidler, Silke Sanderbrandt, Hassan Jomaa, Serge Van Calenbergh, and Andreas Link: Antimalarial Activity of N6-substituted Adenosine Derivatives (Part 3). Bioorg. Med. Chem., 2004, 12, 755-762.



Andreas Link: Combinatorial chemistry as a new approach in antiparasitic drug discovery. Parasitol Res., 2003, 90, Suppl. 2, 86-90.

Tommie L. Lincecum Jr., Michael Tukalo, Anna Yaremchuk, Richard S. Mursinna, Amy M. Williams, Brian S. Sproat, Wendy Van Den Eynde, Andreas Link, Serge Van Calenbergh, Morten Grötli, Susan A. Martinis, and Stephen Cusack: Structural and Mechanistic Basis of Pre- and Posttransfer Editing by Leucyl-tRNA Synthetase. Mol. Cell, 2003, 11, 951-963.



Claudia Herforth, Jochen Wiesner, Stephan Franke, Abolfasl Golisade, Hassan Jomaa, and Andreas Link: Antimalarial Activity of N6-substituted Adenosine Derivatives (Part 2). J. Comb. Chem., 2002, 4, 302-314.

Andreas Link: Dynamite approach to delicate complex scaffolds. Drug Discov. Today 2002, 7, 548-549.

Serge Van Calenbergh, Andreas Link, Shelly Fujikawa, Rianne de Ligt, Veerle Vanheusden, Abolfasl Golisade, Norbert Blaton, Jef Rozenski, Adriaan IJzerman, and Piet Herdewijn: 5'-Deoxy Congeners of 9-(3-Amido-3-deoxy-ß-D-xylofuranosyl)-N6-cyclopentyladenine: New Adenosine A1 Receptor Antagonists and Inverse Agonists. J. Med. Chem., 2002, 45, 1845-1852.

Abolfasl Golisade, Jochen Wiesner, Claudia Herforth, Hassan Jomaa, and Andreas Link: Anti-Malarial Activity of N6-substituted Adenosine Derivatives. Part I. Bioorg. Med. Chem., 2002, 10, 769-777.

Abolfasl Golisade, Claudia Herforth, Ludo Quirijnen, Louis Maes, and Andreas Link: Improving an Antitrypanosomal Lead Applying Nucleophilic Substitution on a Safety Catch Linker, Bioorg. Med. Chem., 2002, 10, 159-165.



Kenneth A. Jacobsen, Zhan-Guo Gao, Aishe Chen, Dov Barak, Soon-Ai Kim, Kyeong Lee, Andreas Link, Philippe Van Rompaey, Serge van Calenbergh, and Bruce T. Liang: Neoceptor Concept Based on Molecular Complementarity in GPCRs: A Mutant Adenosine A3 Receptor with Selectively Enhanced Affinity for Amine-Modified Nucleosides, J. Med. Chem., 2001, 44, 4125-4136.

Abolfasl Golisade, Claudia Herforth, Karen Wieking, Conrad Kunick, and Andreas Link: Biotin Labelling of amines by polymer assisted solution phase synthesis. Bioorg. Med. Chem. Lett., 2001, 11, 1783-1786.

Christiane Schultz, Andreas Link, und Conrad Kunick: Aryl rings are part of the darpone pharmacophore. Arch. Pharm. Pharm. Med. Chem., 2001, 334, 163-166.



Andreas Link: Terminologie der Anwendung temporär gebundener, löslichkeitsmodifizierender Auxiliare in der kombinatorischen Chemie - ein kritischer Kommentar. Angew. Chem., 2000, 112, 4203-4205.

Andreas Link: Comments on the Terminology for Applications of Temporarily Attached Solubility-Modifying Moieties in Combinatorial Chemistry. Angew. Chem. Int. Ed. 2000, 39, 4039-4040.

Maryse Leost, Christiane Schultz, Andreas Link, Yong-Zhong Wu, Jacek Biernat, Eva-Maria Mandelkow, James A. Bibb, Gretchen L. Snyder, Paul Greengard, Daniel W. Zaharevitz, Edward A. Sausville, Conrad Kunick and Laurent Meijer: Paullones are potent inhibitors of glycogen synthase kinase-3/cyclin-dependent kinase 5/p25. Eur. J. Biochem., 2000, 267, 5983-5994.

Abolfasl Golisade, Jerome C. Bressi, Serge Van Calenbergh, Michael H. Gelb, and Andreas Link: Polymer-Assisted Solution Phase Synthesis of 2'-Amido-2'-deoxyadenosine Derivatives Targeted at the NAD+-Binding Sites of Parasite Enzymes, J. Comb. Chem., 2000, 2, 537-544.

Rick Gussio, Daniel W. Zaharevitz, Connor F. McGrath, Nagarajan Pattabiraman, Glen E. Kellogg, Christiane Schultz, Andreas Link, Conrad Kunick, Maryse Leost, Laurent Meijer, and Edward A. Sausville: Structure-based design modifications of the paullone molecular scaffold for cyclin-dependent kinase inhibition. Anti-Cancer Drug Design, 2000, 15, 53-66.

Abolfasl Golisade, Serge Van Calenbergh, and Andreas Link: 2'-Amino-2'-deoxy-N6-(1-naphthylmethyl)adenosine as novel scaffold for a polymer-assisted amidation protocol, Tetrahedron, 2000, 56, 3167-3172.



Christiane Schultz, Andreas Link, Maryse Leost, Daniel W. Zaharevitz, Rick Gussio, Edward A. Sausville, Laurent Meijer, and Conrad Kunick: Paullones, a series of cyclin-dependent kinase inhibitors: Synthesis, Evaluation of CDK1/Cyclin B Inhibition, and in Vitro Antitumor Activity. J. Med. Chem., 1999, 42, 2909-2919.

Andreas Link, Daniel W. Zaharevitz, and Conrad Kunick: Antitumor pyrido[3,2-d][1]benzazepines: Synthesis and in vitro activity of thiophene analogs. Pharmazie, 1999, 54, 163-166.

Serge Van Calenbergh, Andreas Link, Conrad Kunick, and Piet Herdewijn: Exploration of the effect of sterically demanding 3'-amido substitution of 3'-deoxyadenosines towards inhibition of cyclin-dependent kinase 1. Pharmazie, 1999, 54, 727-729 and 892.



Andreas Link, Serge Van Calenbergh, and Piet Herdewijn: Practical method for the parallel synthesis of 2'-amido-2'-deoxyadenosines, Tetrahedron Lett., 1998, 39, 5175-5176.

Theo Lescrinier, Chris Hendrix, Luc Kerremans, Jef Rozenski, Andreas Link, Bart Samyn, Arthur Van Aerschot, Evelyne Lescrinier, Ramon Eritja, Jozef van Beeumen, Piet Herdewijn: DNA-Binding Ligands from Peptide Libraries Containing Unnatural Amino Acids, Chem. Eur. J., 1998, 4, 425-433.

Andreas Link and Conrad Kunick: d-Fused [1]benzazepines with selective in vitro antitumor activity: Synthesis and structure-activity relationships. J. Med. Chem., 1998, 41, 1299-1305.

Andreas Link, Theo Lescrinier, Luc Kerremans, Jef Rozenski, Arthur Van Aerschot, and Piet Herdewijn: Side Reactions in Solid Phase Peptide Synthesis Caused by Sulfonyl-Ornithine Building Blocks, Pharmazie, 1998, 53, 200-201.



Andreas Link, Conrad Kunick: Preparation of spiro[1-benzazepine-4,1'-cyclohexane] derivatives from 1H-1-benzazepine-2,5(3H,4H)-diones and Mannich bases. Synthesis, 1997, 297-300.



Conrad Kunick, Andreas Link und Max Hropot: Synthesis and in vivo testing of a potential aquaretic agent. Pharmazie, 1996, 51, 601-602.



Conrad Kunick, and Andreas Link: Synthesis of Pyrido[3,2-d][1]benzazepines. J. Heterocycl. Chem., 1995, 32, 803-805.